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    Neo-tryptophan
    2.
    发明申请
    Neo-tryptophan 失效
    新色氨酸

    公开(公告)号：US20070173458A1

    公开(公告)日：2007-07-26

    申请号：US11452616

    申请日：2006-06-14

    Applicant: Elliott Richelson ,  Bernadette Cusack ,  Yuan-Ping Pang ,  Daniel McCormick ,  Abdul Fauq ,  Beth Tyler ,  Mona Boules

    Inventor： Elliott Richelson ,  Bernadette Cusack ,  Yuan-Ping Pang ,  Daniel McCormick ,  Abdul Fauq ,  Beth Tyler ,  Mona Boules

    IPC: C07K7/06 ,  A61K38/08

    CPC classification number: C07K7/083 ,  A61K38/00 ,  C07D209/08 ,  C07K7/14 ,  C07K7/18 ,  C07K14/70 ,  C07K14/702

    Abstract: The invention provides a novel amino acid, neo-tryptophan, as well as polypeptides containing this novel amino acid such as neurotensin analogs. In addition, the invention provides neo-tryptophan derivatives, serotonin-like neo-tryptophan derivatives, and polypeptides containing such derivatives. The invention also provides methods for making neo-tryptophan, neo-tryptophan derivatives, serotonin-like neo-tryptophan derivatives, and compositions containing these compounds. Further, the invention provides methods for inducing a neurotensin response in a mammal as well as methods for treating a mammal having a serotonin recognition molecule.

    Abstract translation: 本发明提供了新的氨基酸，新色氨酸，以及含有这种新型氨基酸的多肽，如神经降压素类似物。 此外，本发明提供新色氨酸衍生物，5-羟色胺样新色氨酸衍生物和含有这些衍生物的多肽。 本发明还提供了制备新色氨酸，新色氨酸衍生物，血清素样新色氨酸衍生物和含有这些化合物的组合物的方法。 此外，本发明提供了在哺乳动物中诱导神经降压素反应的方法以及用于治疗具有5-羟色胺识别分子的哺乳动物的方法。

    Neo-tryptophan
    5.
    发明申请
    Neo-tryptophan 有权
    新色氨酸

    公开(公告)号：US20030166505A1

    公开(公告)日：2003-09-04

    申请号：US10265099

    申请日：2002-10-04

    Applicant: Mayo Foundation for Medical Education and Research, a Minnesota corporation

    Inventor： Elliott Richelson ,  Bernadette Marie Cusack ,  Yuan-Ping Pang ,  Daniel J. McCormick ,  Abdul Fauq ,  Beth Marie Tyler ,  Mona Boules

    IPC: A61K038/16 ,  C07K014/435 ,  C07K007/08 ,  C12Q001/37 ,  G01N033/53 ,  C07D209/20

    CPC classification number: C07K7/083 ,  A61K38/00 ,  C07D209/08 ,  C07K7/14 ,  C07K7/18 ,  C07K14/70 ,  C07K14/702

    Abstract: The invention provides a novel amino acid, neo-tryptophan, as well as polypeptides containing this novel amino acid such as neurotensin analogs. In addition, the invention provides neo-tryptophan derivatives, serotonin-like neo-tryptophan derivatives, and polypeptides containing such derivatives. The invention also provides methods for making neo-tryptophan, neo-tryptophan derivatives, serotonin-like neo-tryptophan derivatives, and compositions containing these compounds. Further, the invention provides methods for inducing a neurotensin response in a mammal as well as methods for treating a mammal having a serotonin recognition molecule.

    Abstract translation: 本发明提供了新的氨基酸，新色氨酸，以及含有这种新型氨基酸的多肽，如神经降压素类似物。 此外，本发明提供新色氨酸衍生物，5-羟色胺样新色氨酸衍生物和含有这些衍生物的多肽。 本发明还提供了制备新色氨酸，新色氨酸衍生物，血清素样新色氨酸衍生物和含有这些化合物的组合物的方法。 此外，本发明提供了在哺乳动物中诱导神经降压素反应的方法以及用于治疗具有5-羟色胺识别分子的哺乳动物的方法。

    Peptide, a method for its preparation and a pharmaceutical composition containing the peptide
    6.
    发明授权
    Peptide, a method for its preparation and a pharmaceutical composition containing the peptide 失效
    肽，其制备方法和含有肽的药物组合物

    公开(公告)号：US06184208B2

    公开(公告)日：2001-02-06

    申请号：US08681248

    申请日：1996-07-22

    Applicant: Vladislav I. Deigin ,  Yelena Yarova

    Inventor： Vladislav I. Deigin ,  Yelena Yarova

    IPC: A61K3800

    CPC classification number: C07K5/1016 ,  A61K38/00 ,  C07K14/702

    Abstract: A peptide of the formula I X-Tyr-Y-Phe-Z-A  I wherein X is hydrogen, arginine, D-arginine, ornithine, D-ornithine, lysine, D-lysine, homoarginine, D-homoarginine, citrulline, D-citrulline; Tyr is tyrosine; Y is D-alanine, D-valine, D-leucine, D-isoleucine, D-phenylalanine, D-asparagine, D-tryptophan, D-proline, D-serine, D-threonine, D-tyrosine, D-hydroxyproline, D-cysteine, D-cysteyl-cysteine, D-methionine, D-lysine, D-homoarginine, D-arginine, D-histidine, D-aspartic acid, D-glutamic acid, D-&bgr;-alanine, or D-ornithine; Phe is phenylalanine; Z is alanine, D-alanine, valine, D-valine, leucine, D-leucine, isoleucine, D-isoleucine, phenylalanine, D-phenylalanine, asparagine, D-asparagine, glycine, glutamine, D-glutamine, tryptophan, D-tryptophan, proline, D-proline, serine, D-serine, threonine, D-threonine, tyrosine, D-tyrosine, hydroxyproline, D-hydroxyproline, cysteine, D-cysteine, cysteyl-cysteine, cysteine-D-cysteine, D-cysteyl-cysteine, D-cysteine-D-cysteine, methionine, D-methionine, lysine, D-lysine, arginine, D-arginine, histidine, D-histidine, aspartic acid, D-aspartic acid, glutamic acid, D-glutamic acid, &bgr;-alanine, D-&bgr;-alanine, ornithine, or D-ornithine; and A is hydroxyl or substituted amide (C1-C3); compositions containing same and its use in modulating physiological processes such as weight gain, activities of the epithelium growth zone, hair growth, wound healing, and to stimulate reparative and anabolic processes, and exert analgesic effects.

    Abstract translation: 式I的肽，其中X是氢，精氨酸，D-精氨酸，鸟氨酸，D-鸟氨酸，赖氨酸，D-赖氨酸，高精氨酸，D-高精氨酸，瓜氨酸，D-瓜氨酸; Tyr是酪氨酸; Y是D-丙氨酸，D-缬氨酸，D-亮氨酸，D-异亮氨酸，D-苯丙氨酸，D-天冬酰胺，D-色氨酸，D-脯氨酸，D-丝氨酸，D-苏氨酸，D-酪氨酸，D-羟脯氨酸， D-半胱氨酸，D-半胱氨酰半胱氨酸，D-甲硫氨酸，D-赖氨酸，D-高精氨酸，D-精氨酸，D-组氨酸，D-天冬氨酸，D-谷氨酸，D-β-丙氨酸或D-鸟氨酸 ; Phe是苯丙氨酸; Z是丙氨酸，D-丙氨酸，缬氨酸，D-缬氨酸，亮氨酸，D-亮氨酸，异亮氨酸，D-异亮氨酸，苯丙氨酸，D-苯丙氨酸，天冬酰胺，D-天冬酰胺，甘氨酸，谷氨酰胺，D-谷氨酰胺，色氨酸， 色氨酸，脯氨酸，D-脯氨酸，丝氨酸，D-丝氨酸，苏氨酸，D-苏氨酸，酪氨酸，D-酪氨酸，羟脯氨酸，D-羟脯氨酸，半胱氨酸，D-半胱氨酸，半胱氨酰半胱氨酸，半胱氨酸-D-半胱氨酸， 半胱氨酸 - 半胱氨酸，D-半胱氨酸-D-半胱氨酸，甲硫氨酸，D-甲硫氨酸，赖氨酸，D-赖氨酸，精氨酸，D-精氨酸，组氨酸，D-组氨酸，天冬氨酸，D-天冬氨酸，谷氨酸，D-谷氨酸 酸，β-丙氨酸，D-β-丙氨酸，鸟氨酸或D-鸟氨酸; 和A是羟基或取代的酰胺（C1-C3）; 含有该组合物的组合物及其在调节生理过程中的用途，例如体重增加，上皮生长区的活性，毛发生长，伤口愈合，以及刺激修复和合成代谢过程，并发挥镇痛作用。

    Peptides and therapeutic applications thereof
    8.
    发明授权
    Peptides and therapeutic applications thereof 失效
    肽及其治疗应用

    公开(公告)号：US4407794A

    公开(公告)日：1983-10-04

    申请号：US289383

    申请日：1981-08-03

    Applicant: Bernard Roques ,  Jeanne-Marie Lecomte

    Inventor： Bernard Roques ,  Jeanne-Marie Lecomte

    IPC: C07K14/655 ,  A61K38/00 ,  A61P25/00 ,  C07K7/06 ,  C07K14/575 ,  C07K14/67 ,  C07K14/70 ,  A61K37/00 ,  C07C103/52

    CPC classification number: C07K14/672 ,  C07K14/702 ,  A61K38/00 ,  Y10S514/809

    Abstract: This invention relates to peptide derivatives of the formula:Tyr--A--Gly--B--C--D (I)in which:A is a D.Ala, AzaGly, Aib, D.Ser., D.Thr, D.Cys, homo Serine, .beta.Phe Ser, .beta.OH Leu, 4OH Ile, .alpha.,.beta.,.gamma. OHNor Val or OH Val residue in which the side-chain OH or SH groups, when same exist, may be free or protected (i) by a straight- or branched-chain alkyl containing 1-6 carbon atoms, (ii) by an unsubstituted phenyl radical or a phenyl radical substituted with one or more fluorine atoms, (iii) by an unsubstituted benzyl radical or a benzyl radical substituted with one or more fluorine atoms, (iv) by an aliphatic acyl radical having 1-6 carbon atoms or an acyl radical COX in which X is a phenyl, benzyl or benzhydryl radical, optionally substituted with one or more fluorine atoms,B is a L.Phe, pF.L.Phe or pentafluoro L.Phe residue,C is a Leu, N.Leu or Ile residue of D or L configuration,D is hydrogen or a group of the formula: ##STR1## in which n=0, 1 or 2, R is a hydrogen atom or a radical as defined for the protection of group OH of residue A,Y is a hydrogen atom, a group hydroxy, carboxy, carbamoyl, a group OR.sub.1, COOR.sub.1 or CONHR.sub.1 in which R.sub.1 represents a radical as defined for the protection of group OH of residue A, a phosphatidylethanolamine chain or a chain ##STR2## in which n is an integer from 0 to 3, R.sub.2 is a hydrogen atom or a straight alkyl radical containing 1-4 carbon atoms, and R.sub.3 is a hydrogen or oxygen atom or a straight alkyl residue containing 1-4 carbon atoms,and their pharmaceutically acceptable salts.Said compounds are therapeutically useful, typically an analgesic, psychotropic and anti-diarrheic agents.

    Abstract translation: 本发明涉及下式的肽衍生物：Tyr-A-Gly-BCD（I），其中：A为D.Ala，AzaGly，Aib，D.Ser。，D.Thr，D.Cys，高丝氨酸， βPhe Ser，βOH Leu，4OH Ile，α，β，γOHNor Val或OH Val残基，其中侧链OH或SH基团当存在时可以是游离的或受保护的（i）通过直链或 含有1-6个碳原子的支链烷基，（ii）未取代的苯基或被一个或多个氟原子取代的苯基，（iii）未取代的苄基或被一个或多个氟原子取代的苄基 ，（iv）具有1-6个碳原子的脂族酰基或酰基COX，其中X是苯基，苄基或二苯甲基，任选被一个或多个氟原子取代，B是L.Phe，pF。 L.Phe或五氟L.Phe残基，C是D或L构型的Leu，N.Leu或Ile残基，D是氢或下式的基团：其中n = 0,1或2， R是氢原子 如保护残基A的OH基团所定义的基团，Y是氢原子，羟基，羧基，氨基甲酰基，基团OR1，COOR1或CONHR1，其中R1表示为保护基团OH定义的基团 残基A，磷脂酰乙醇胺链或NH（CH2）nR3NR2R2 + RF，其中n为0-3的整数，R2为氢原子或含有1-4个碳原子的直链烷基，R3为氢或 氧原子或含有1-4个碳原子的直链烷基，及其药学上可接受的盐。 所述化合物是治疗上有用的，通常是镇痛药，精神药物和抗腹泻剂。

    Enkephalin analogs and a process for the preparation thereof
    9.
    发明授权
    Enkephalin analogs and a process for the preparation thereof 失效
    脑啡肽类似物及其制备方法

    公开(公告)号：US4339440A

    公开(公告)日：1982-07-13

    申请号：US227766

    申请日：1981-01-23

    Applicant: Sandor Bajusz ,  Andras Ronai ,  Jozsef Szekely

    Inventor： Sandor Bajusz ,  Andras Ronai ,  Jozsef Szekely

    IPC: A61K38/00 ,  A61K38/22 ,  A61P9/12 ,  A61P25/04 ,  A61P25/30 ,  C07C67/00 ,  C07C231/00 ,  C07F9/38 ,  C07K5/087 ,  C07K5/10 ,  C07K5/107 ,  C07K14/575 ,  C07K14/655 ,  C07K14/70 ,  A61K37/00 ,  C07C103/52

    CPC classification number: C07K14/702 ,  C07F9/3808 ,  C07K5/0812 ,  C07K5/1016 ,  C07K5/1027 ,  A61K38/00 ,  Y02P20/55 ,  Y10S514/80

    Abstract: The invention relates to new enkephalin analogues of the general formula (I),Tyr-X-Gly-Phe-Y (I)whereinTyr, Gly and Phe represent L-tyrosyl, glycyl and L-phenylalanyl residue, respectively,X is glycyl residue or a D-.alpha.-aminocarboxylic acid residue with a lower alkyl, lower thioalkyl or phenyl-(lower)-alkyl side chain, andY is the residue of an L, D or DL-.alpha.-aminophosphonic acid or L, D or DL-.alpha.-aminosulfonic acid, each having a lower alkyl side chain,and salts thereof. These compounds are prepared according to the invention so that an L-, D- or DL-.alpha.-aminophosphonic acid or an L-, D- or DL-.alpha.-aminosulfonic acid, each bearing a lower alkyl side chain, is coupled in the proper order, as defined by formula (I), with the amino acids and/or peptide fragments each having a removable protecting group on the terminal amino group, the protecting group is split off from the terminal amino group, and the free peptide is isolated as such or in the form of its salt.The new compounds according to the invention selectively modify the catecholamine content of the central nucleus of amygdala, thus they may specifically influence the following functions: food intake, emotionality, social behavior, learning and memory processes.

    Abstract translation: 本发明涉及通式（I）的新型脑啡肽类似物，Tyr-X-Gly-Phe-Y（I），其中Tyr，Gly和Phe分别代表L-酪氨酰基，甘氨酰和L-苯丙氨酰残基，X是甘氨酰 残基或具有低级烷基，低级硫代烷基或苯基 - （低级） - 烷基侧链的D-α-氨基羧酸残基，Y是L，D或DL-α-氨基膦酸或L，D或 各自具有低级烷基侧链的DL-α-氨基磺酸及其盐。 根据本发明制备这些化合物，使得每个具有低级烷基侧链的L-，D-或DL-α-氨基膦酸或L-，D-或DL-α-氨基磺酸在 由式（I）定义的适当顺序，氨基酸和/或肽片段在末端氨基上各自具有可除去的保护基，保护基与末端氨基分离，游离肽被分离 本身或其盐的形式。 根据本发明的新化合物选择性地改变杏仁核中心核的儿茶酚胺含量，因此它们可以具体影响以下功能：食物摄入，情绪，社会行为，学习和记忆过程。

    2,6-C-Dimethyltyrosine.sup.1 -D-amino acid.sup.2 -.epsilon.-amino caproic and .gamma. aminobutyric acid.sup.5 derivatives of methionine enkephalin
    10.
    发明授权
    2,6-C-Dimethyltyrosine.sup.1 -D-amino acid.sup.2 -.epsilon.-amino caproic and .gamma. aminobutyric acid.sup.5 derivatives of methionine enkephalin 失效
    2,6-C-二甲基酪氨酸1-D-氨基酸2-ε-氨基己酸和γ-氨基丁酸5甲硫氨酸脑啡肽的衍生物

    公开(公告)号：US4316892A

    公开(公告)日：1982-02-23

    申请号：US202920

    申请日：1980-11-03

    Applicant: David A. Jones

    Inventor： David A. Jones

    IPC: C07K14/655 ,  A61K38/00 ,  A61K38/22 ,  A61P25/04 ,  C07K7/02 ,  C07K14/575 ,  C07K14/70 ,  A61K37/00 ,  C07C103/52

    CPC classification number: C07K7/02 ,  C07K14/702 ,  A61K38/00 ,  Y10S514/809

    Abstract: An enkephalin derivative represented by the formula(.+-.) H-2,6-C-diMeTyr-(D)X-Gly-Phe-N(CH.sub.2).sub.m COORwherein: X is methionine, alanine or nor-leucine; m is 3 or 5; and R is selected from the group consisting of hydrogen, lower alkyl or -NR.sub.2 R.sub.3 wherein R.sub.2 and R.sub.3 are the same or different members of the group consisting of hydrogen and lower alkyl, wherein the (.+-.) refers to the compound shown, its mirror image or a mixture of racemates; or the pharmaceutically acceptable salts thereof. The compounds are useful as analgesic agents.

    Abstract translation: 由式（+/-）H-2,6-C-diMeTyr-（D）X-Gly-Phe-N（CH 2）m COOR表示的脑啡肽衍生物，其中：X是甲硫氨酸，丙氨酸或不亮氨酸; m为3或5; 并且R选自氢，低级烷基或-NR 2 R 3，其中R 2和R 3是由氢和低级烷基构成的组中相同或不同的成员，其中（+/-）是指所示的化合物，其 镜像或外来物质的混合物; 或其药学上可接受的盐。 该化合物可用作止痛剂。

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